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  1. GPCR drug discovery: new agents, targets and indications - Nature

    We find that there are 516 approved drugs targeting GPCRs, making up 36% of all approved drugs. These drugs act on 121 GPCR targets, one-third of all non-sensory GPCRs. Furthermore, 337...

  2. Key aspects of modern GPCR drug discovery - ScienceDirect

    Jan 1, 2024 · G-protein-coupled receptors (GPCRs) are the largest and most versatile cell surface receptor family with a broad repertoire of ligands and functions. …

  3. GPCR Drug Discovery: New Drugs, New Targets, and New Indications

    Apr 17, 2025 · G protein-coupled receptors (GPCRs) remain one of the most valuable and versatile classes of drug targets in modern medicine. This blog explores the evolving landscape of GPCR drug …

  4. Structure, function and drug discovery of GPCR signaling

    Dec 4, 2023 · Their diverse and essential roles in the body make them a significant focus for pharmaceutical research and drug development. Currently, approximately 35% of marketed drugs …

  5. An online GPCR drug discovery resource - bioRxiv

    Jan 11, 2025 · Altogether, this tool informs of 162 the current status of specific GPCRs as drug targets pinpoints both those being re-targeted and entering 163 clinical trials for the first time.

  6. Pharmacogenomics of GPCR Drug Targets: Cell

    A pharmacogenomic analysis probes the effects of genetic variation in G-protein-coupled receptors on responses to FDA-approved drugs and estimates how this genetic variation may impact healthcare …

  7. GPCRs: Structures, Research Trends, and Landscape - Excelra

    GPCRs are the largest family of proteins involved in membrane signal transduction and are also the most intensively studied drug targets, largely due to their substantial involvement in human …

  8. G-Protein coupled receptors (GPCRs) and their role in targeted drug ...

    Nov 10, 2021 · In this article, signaling pathways, the structure of GPCRs and the development pattern of different stages of targeted drugs are covered.

  9. Frontiers | Accelerating GPCR Drug Discovery With Conformation ...

    May 23, 2022 · GPCRs transduce extracellular stimuli into a plethora of vital physiological processes. Consequently, GPCRs are an attractive drug target class. This is underlined by the fact that …

  10. GPCR drug discovery: new agents, targets and indications.

    Mar 3, 2025 · We find that there are 516 approved drugs targeting GPCRs, making up 36% of all approved drugs. These drugs act on 121 GPCR targets, one-third of all non-sensory GPCRs. …